G Protein Coupled Receptors And Structure-Based Advances

Title:G Protein Coupled Receptors And Structure-Based Advances

Volume: 16 Issue: 13

Author(s): Maria Kontoyianni

Affiliation:

Keywords: G Protein Coupled Receptors, Homology Modeling, Virtual Screening, Model-Building, Critical Assessment of Structure Prediction, Docking, Structure-Based Drug Design, Activation Mechanisms, Conserved Motifs.

Abstract: G protein coupled receptors (GPCRs) are membrane proteins coupled with G proteins through which they transmit signals to the cytoplasm. Approximately 30% of pharmaceuticals target these receptors, even though crystal structures were scarce at the time. Furthermore, an additional 15% of GPCRs have yet to be exploited for therapeutic intervention. An overview of structural information is presented, with emphasis on rearrangements occurring during activation,in light of recently resolved activated state crystal structures. Computational efforts over recent years are also highlighted.

Cite this article as:

Kontoyianni Maria, G Protein Coupled Receptors And Structure-Based Advances, Current Topics in Medicinal Chemistry 2016; 16 (13) . https://dx.doi.org/10.2174/1568026615666150915121324